Assay Detail
Binding
CHEMBL4122799
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length recombinant His6-tagged human PARP14 WWA/catalytic domain expressed in Escherichia coli BL21(DE3) preincubated for 15 mins followed by biotinylated NAD+ addition by chemiluminescence assay
30
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Protein mono-ADP-ribosyltransferase PARP14 (CHEMBL2176777) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis and evaluation of potent and selective inhibitors of mono-(ADP-ribosyl)transferases PARP10 and PARP14.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 5.59 | 6.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4126260 | — | — | 2 | 6.16 |
| CHEMBL4129001 | — | — | 2 | 6.11 |
| CHEMBL4126241 | — | — | 2 | 5.98 |
| CHEMBL4127497 | — | — | 2 | 5.97 |
| CHEMBL4125748 | — | — | 2 | 5.89 |
| CHEMBL4128574 | — | — | 2 | 5.84 |
| CHEMBL4127327 | — | — | 2 | 5.62 |
| CHEMBL4129542 | — | — | 2 | 5.50 |
| CHEMBL4128256 | — | — | 2 | 5.44 |
| CHEMBL4127476 | — | — | 2 | 5.38 |
| CHEMBL4129782 | — | — | 2 | 5.33 |
| CHEMBL4130035 | — | — | 2 | 5.32 |
| CHEMBL4129789 | — | — | 2 | 5.28 |
| CHEMBL4126166 | — | — | 2 | 5.24 |
| CHEMBL1438938 | — | — | 2 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4126260 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4126260 | — | IC50 | = | 691.83 | nM | 6.16 |
| CHEMBL4129001 | — | IC50 | = | 776.25 | nM | 6.11 |
| CHEMBL4129001 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL4126241 | — | IC50 | = | 1047.13 | nM | 5.98 |
| CHEMBL4127497 | — | IC50 | = | 1071.52 | nM | 5.97 |
| CHEMBL4125748 | — | IC50 | = | 1288.25 | nM | 5.89 |
| CHEMBL4125748 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4126241 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4128574 | — | IC50 | = | 1445.44 | nM | 5.84 |
| CHEMBL4128574 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4127497 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4127327 | — | IC50 | = | 2398.83 | nM | 5.62 |
| CHEMBL4127327 | — | IC50 | = | 2430.0 | nM | 5.61 |
| CHEMBL4129542 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4129542 | — | IC50 | = | 3235.94 | nM | 5.49 |
| CHEMBL4128256 | — | IC50 | = | 3630.78 | nM | 5.44 |
| CHEMBL4128256 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL4127476 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL4127476 | — | IC50 | = | 4265.8 | nM | 5.37 |
| CHEMBL4129782 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL4129782 | — | IC50 | = | 4677.35 | nM | 5.33 |
| CHEMBL4130035 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL4130035 | — | IC50 | = | 4786.3 | nM | 5.32 |
| CHEMBL4129789 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL4129789 | — | IC50 | = | 5248.07 | nM | 5.28 |
| CHEMBL4126166 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL4126166 | — | IC50 | = | 5754.4 | nM | 5.24 |
| CHEMBL1438938 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL1438938 | — | IC50 | = | 10000.0 | nM | 5.00 |